Robertson B, Owen D, Stow J, Butler C, Newland C
Department of Biochemistry, Imperial College of Science, Technology and Medicine, London, UK.
FEBS Lett. 1996 Mar 25;383(1-2):26-30. doi: 10.1016/0014-5793(96)00211-6.
We have examined the effects of two DTX homologues, toxin I and toxin K, on Kv1.1, Kv1.2 and Kv1.6 channels expressed in Xenopus oocytes. Toxin I blocked all three channels; in contrast, toxin K was selective for Kv1.1. Both toxins slowed channel activation and inactivation kinetics with 10 nM toxin I approximately doubling activation and inactivation time constants of Kv1.1. For the first time, we have demonstrated the selectivity of a DTX homologue for a single cloned Kv1 channel and suggest that these toxins may sterically hinder the conformational changes that occur during channel gating.
我们研究了两种DTX同源物毒素I和毒素K对非洲爪蟾卵母细胞中表达的Kv1.1、Kv1.2和Kv1.6通道的影响。毒素I阻断了所有这三种通道;相比之下,毒素K对Kv1.1具有选择性。两种毒素均减慢了通道激活和失活动力学,10 nM毒素I使Kv1.1的激活和失活时间常数增加了约一倍。我们首次证明了一种DTX同源物对单个克隆的Kv1通道具有选择性,并表明这些毒素可能在空间上阻碍通道门控过程中发生的构象变化。